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1.
РЖ ВИНИТИ 76 (BI28) 95.08-04Н3.026

    Kaltenbach, Matthieu L.

    KINFIT: a non linear Least-Squares Computer Program for the Estimation of Pharmacokinetic Parameters after Intravenous Administration [Text] : [Pap.] 5th Conf. Oncol. Clin. Pharmacol., Reims, 8-10 Nov., 1994 / Matthieu L. Kaltenbach, Richard Vistelle // Anticancer. Res. - 1994. - Vol. 14, N 6А. - P2375-2377 . - ISSN 0250-7005
Перевод заглавия: KINFIT: нелинейная компъютерная программа с методом наименьших квадратов для оценки фармакокинетических параметров после внутривенного введения
Аннотация: KINFIT is a nonlinear least-squares computer program designed to allow pharmacokinetic modeling of experimental data and to obtain pertinent parameter estimates based on the derived values. It is written in Visual BASIC for the Microsoft Windows graphical environment. Drug concentrations in blood, plasma, or serum with time following intravenous administration are input and a linear or semi-logarithmic plot of the data appears on the display. On command, polyexponential coefficients and exponents are computed and a non linear curve is fitted through the data set. Results from statistical tests are printed to determine goodness of fit. Commonly calculated pharmacokinetic parameters are also calculated and appear on the output. The execution of KINFIT is demonstrated for time courses of ampicillin in man. KINFIT was compared with the widely available ESTRIP and RSTRIP computer programs and gave parameter estimates that were very similar, although not identical. Ил. 3. Табл. 2. Библ. 13.
ГРНТИ  
ВИНИТИ 761.29.49.55.07.05
Рубрики: ЛЕКАРСТВЕННЫЕ СРЕДСТВА
ФАРМАКОКИНЕТИЧЕСКИЕ ПАРАМЕТРЫ

КОМПЬЮТЕРНАЯ ПРОГРАММА


Доп.точки доступа:
Vistelle, Richard

2.
РЖ ВИНИТИ 76 (BI31) 95.10-04Т3.7

   

    Pharmacokinetics of acetylsalicylic acid and its metabolites at low doses: A compartmental modeling [Text] / D. Dubovska [et al.] // Meth. and Find. Exp. and Clin. Pharmacol. - 1995. - Vol. 17, N 1. - P67-77 . - ISSN 0379-0355
Перевод заглавия: Фармакокинетика ацетилсалициловой кислоты и ее метаболитов в низких дозах: раздельное моделирование
Аннотация: The pharmacokinetics of acetylsalicylic acid (ASA) and its metabolites salycylic acid (SA) and salicyluric acid (SUA) were studied in 12 healthy young volunteers after oral administration of low (30 and 100 mg) and moderate (400 mg) doses. Plasma and urine were assayed for the above drugs by high-performance liquid chromatographic method. Individual pharmacokinetic parameters were estimated by compartmental modeling (ASA and SA) and by model-independent methods (SUA). ASA parameter values estimated in this study were in agreement with those reported by other authors after administration of higher doses, which confirms the linearity of ASA pharmacokinetics in a broad dose range. On the contrary, both metabolic and renal elimination routes for SA were found to be saturable. The relative changes in SA renal clearance with the dose were more pronounced than those in metabolic clearance. Particularly, there was no statistically significant difference in SA metabolic clearance between 30 and 100 mg doses, indicating linear kinetics in this dose range. Further increase in the dose resulted in significant decrease in SA metabolic clearance. At the same time, both SA excretion rate constant and fraction excreted significantly diminished across the entire dose range studied. The dependence of SUA renal clearance upon the dose was shown to be complex, reflecting possible saturability of its excretion
ГРНТИ  
ВИНИТИ 761.31.29.02.09
Рубрики: ФАРМАКОКИНЕТИКА
КИСЛОТА АЦЕТИЛСАЛИЦИЛОВАЯ

МЕТАБОЛИТЫ

ДОЗЫ

ФАРМАКОКИНЕТИЧЕСКИЕ ПАРАМЕТРЫ

КРОВЬ

МОЧА

ЗДОРОВЫЕ ИСПЫТУЕМЫЕ


Доп.точки доступа:
Dubovska, D.; Piotrovskij, V.K.; Gajdos, M.; Krivosikova, Z.; Spustova, V.; Trnovec, T.

3.
РЖ ВИНИТИ 76 (BI31) 95.10-04Т3.8

   

    Pharmacokinetic studies in healthy volunteers on a new gastroprotective pharmaceutic form of diclofenac [Text] / Bernardi di Valserra M. De [et al.] // Arzneim.-Forsch. - 1993. - Vol. 43, N 3. - P373-377 . - ISSN 0004-4172
Перевод заглавия: Фармакокинетическое исследование новой гастропротекторной фармацевтической формы диклофенака у здоровых испытуемых
Аннотация: The pharmacokinetic properties of a new gastroprotective pharmaceutical formulation of diclofenac (CAS 15307-79-6) were investigated in twelve healthy volunteers. In this new form the diclofenac is the nucleus of sequential sucralfate-covered tablets. The experimental design was an open, random, two period balanced crossover study. All the subjects received a single oral dose of 50 mg diclofenac contained in the new formulation or in the reference enteric-coated tablets. Plasma concentrations of diclofenac were determined at 0.5 1, 2, 4, 6, and 8 h after drug administration using HPLC method. After administration of a diclofenac-sucralfate association diclofenac was quickly adsorbed and the peak plasma concentration (0.733'+-'0.08 'мю'g/ml) was achieved in about 1 h. AUC[(0-'БЕСКОНЕЧН')] value was about 1.8 'мю'g/ml/h and the mean elimination half-life was 1.20'+-'0.12 h. The pharmacokinetic profile of diclofenac-sucralfate association is similar to the values reported in previous papers for enteric-coated forms; anyway an early accurrence of the peak plasma concentration was observed for the new formulation. The new diclofenac-sucralfate association shows a different rate of absorption (namely an early and greater peak plasma concentration of diclofenac) and a similar extent of absorption (AUC[(0-'БЕСКОНЕЧН')] being not statisctically different) as compared to the reference enteric-coated tablets of 50 mg diclofenac. These results could be related to the delaying and protective effect of sucralfate whose action is different from the one carried by the coat of the enteric-coated tablets
ГРНТИ  
ВИНИТИ 761.31.29.02.09
Рубрики: ФАРМАКОКИНЕТИКА
ДИКЛОФЕНАК

НОВАЯ ЛЕКАРСТВЕННАЯ ФОРМА

ДОЗЫ

ФАРМАКОКИНЕТИЧЕСКИЕ ПАРАМЕТРЫ

ЗДОРОВЫЕ ИСПЫТУЕМЫЕ


Доп.точки доступа:
De, Bernardi di Valserra M.; Feletti, F.; Tripodi, A.S.; Contos, S.; Carabelli, A.; Maggi, L.; Germogli, R.

4.
РЖ ВИНИТИ 76 (BI31) 95.10-04Т3.9

   

    Pharmacokinetics and tolerance of fluconazole suppositories in healthy volunteers [Text] / G. Pfaff [et al.] // Arzneim.-Forsch. - 1993. - Vol. 43, N 3. - P391-395 . - ISSN 0004-4172
Перевод заглавия: Фармакокинетика и толерантность суппозиториев флуконазола у здоровых испытуемых
Аннотация: Fluconazole (Diflucan{R}, CAS 86386-73-4) suppositories offer a novel way to administer this systemically active antimycotic. The pharmacokinetics and toleration of this new formulation have now been examined in healthy adult volunteers. In crossover experiments the bioequivalence was demonstrated for 200 mg suppositories and 200 mg capsules, and for 25 mg suppositories and 25 mg fluconazole in an oral suspension. The mean bioavailability of the 200 mg suppository relative to the capsule was about 93%. The mean bioavailability of the 25 mg suppository relative to the oral suspension was 107%. Absorption of fluconazole after administration of the suppositories was, however, somewhat slower than after oral ingestion of the capsule or suspension. The pharmacokinetic parameters of the 200 mg and 25 mg suppositories suggest that the kinetics of rectally administered fluconazole are linear with dosage. Daily administration of the 200 mg suppository gives a continuous increase in the mean fluconazole plasma concentration, until steady-state is reached on about the 5th day. The systemic and local toleration of the fluconazole suppositories was good
ГРНТИ  
ВИНИТИ 761.31.29.02.09
Рубрики: ФАРМАКОКИНЕТИКА
ФЛУКОНАЗОЛ

СУППОЗИТОРИИ

КАПСУЛЫ

ПЕРОРАЛЬНАЯ СУСПЕНЗИЯ

ДОЗЫ

БИОЭКВИВАЛЕНТНОСТЬ

ФАРМАКОКИНЕТИЧЕСКИЕ ПАРАМЕТРЫ

СРАВНИТЕЛЬНЫЙ АНАЛИЗ

ЗДОРОВЫЕ ИСПЫТУЕМЫЕ


Доп.точки доступа:
Pfaff, G.; Zimmermann, T.; Lach, P.; Yeates, R.; Simon, G.; Wildfeuer, A.

5.
РЖ ВИНИТИ 76 (BI31) 95.10-04Т3.10

   

    Relative bioavailability of oral dosage forms of tenoxicam [Text] / T. W. Guentert [et al.] // Arzneim.-Forsch. - 1994. - Vol. 44, N 9. - P1051-1054 . - ISSN 0004-4172
Перевод заглавия: Сравнительная биоэквивалентность пероральных дозированных форм теноксикама
Аннотация: The bioavailability of tenoxicam (Ro 12-0068, Tilcotil{R}, CAS 59804-37-4) from an effervescent tablet and an instant milk drink formulation relative to the commercial 20 mg tablet was investigated in a randomized cross-over study. Twelve healthy male volunteers (age 18-35 years; weight 63-95 kg) received on three different occasions a single oral tablet, an effervescent tablet or an instant milk drink (dissolved in water) with each dose containing 20 mg of tenoxicam. The wash-out period between two consecutive treatments was at least 5 weeks. Plasma concentrations after dosing were determined with a specific HPLC method. With the effervescent tablet and the milk drink, maximum concentrations were obtained at the same time (0.5-3.0 h) as with the reference tablet (0.5-4.0 h). Plasma peak concetrations appeared highest after the commercial tablet (mean'+-'SD: C[max]2.8'+-'0.55 mg/l) but the difference to the effervescent tablet (2.7'+-'0.41 mg/l) and the milk formulation (2.5'+-'0.41 mg/l) was negligible. Similar mean elimination half-lives of 73, 77, and 77 h were obtained with the effercescent tablet, the milk drink, and the commercial tablet, respectively. Average bioavailability relative to the tablet was for the effervescent tablet and for the milk drink 96% with a coefficient of variation of 8%. The 90%-confidence intervals of the mean differences between the test and standard preparations in log-transformed AUC[0-'БЕСКОНЕЧН'] and C[max] were within 20% around the respective mean parameter value calculated for the standard preparation allowing to conclude bioequivalence of the three oral formulations
ГРНТИ  
ВИНИТИ 761.31.29.02.09
Рубрики: ФАРМАКОКИНЕТИКА
ТЕНОКСИКАМ

РАЗЛИЧНЫЕ ПЕРОРАЛЬНЫЕ ФОРМЫ

ФАРМАКОКИНЕТИЧЕСКИЕ ПАРАМЕТРЫ

БОЛЬНЫЕ


Доп.точки доступа:
Guentert, T.W.; Stebler, T.; Banken, L.; Defoin, R.; Schmitt, M.

6.
РЖ ВИНИТИ 76 (BI31) 95.10-04Т3.11

   

    Absolute bioverfugbarkeit von Folsaure nach einmaliger oraler Gabe einer Folsaure-Tablettenzubereitung an gesunde Versuchspersonen [Text] / A. Menke [et al.] // Arzneim.-Forsch. - 1994. - Vol. 44, N 9. - S1063-1067 . - ISSN 0004-4172
Перевод заглавия: Абсолютная биоэквивалентность фолиевой кислоты при приеме внутрь таблеток у здоровых испытуемых
Аннотация: 5 mg folic acid were administered in two sessions to 9 female and 8 male healthy subjects within a balanced 2-way crossover trial either as one Folsan{R} tablet (CAS 59-30-3, test preparation A) or as 2.5 ml of an injection solution (Folsan{R} 2, reference preparation B). Folic acid was determined in serum and urine collected in fractions over 12 h after administration by means of a radioassay. Before each session a saturation period of 9 days duration was performed by administering 1 tablet per day containing 5 mg folic acid followed by a 4-day wash-out period. The mean predose serum level of folic acid amounted to 17.9'+-'5.62 ng/ml before the oral and 18.2'+-'5.73 ng/ml before the intravenous administration. The post dose serum levels were corrected with the individual predose levels. After oral administration of test preparation A a mean peak serum concentration of 243'+-'33.0 ng/ml (C[max]) was obtained after 2.24'+-'0.85 h (t[max]). The mean area under the corrected serum level time curve was determined with 1160'+-'177 ng* h/ml (AUC[(0-12)]). 6 min after intravenous administration serum levels ranged from 559 to 1490 ng/ml. Following correction with the individual predose levels the mean area under the curve amounted to 1550'+-'249 ng* h/ml. The individual bioavailability ratios of AUC[(0-12)] (A versus B) varied between 49.3% and 96.7%. The mean absolute bioavailability of folic acid was 76.2% '+-' 13.8%. Following oral administration of 5 mg folic acid 3180'+-'1050 'мю'g (range: 1760-5640 'мю'g) folic acid was renally excreted in mean during the 0-12 h interval. The respective mean excretion following 5 mg folic acid i.v. amounted to 3830'+-'1090 'мю'g (range: 1520-5860 'мю'g). Based upon urine excretion the mean absolute bioavailability of folic acid from the tablet was 93.0%'+-'47.2% (ns)
ГРНТИ  
ВИНИТИ 761.31.29.02.09
Рубрики: ФАРМАКОКИНЕТИКА
ФОЛИЕВАЯ КИСЛОТА

ТАБЛЕТКИ

РАСТВОР

ФАРМАКОКИНЕТИЧЕСКИЕ ПАРАМЕТРЫ

КРОВЬ

МОЧА

ЗДОРОВЫЕ ИСПЫТУЕМЫЕ


Доп.точки доступа:
Menke, A.; Weimann, H.-J.; Achtert, G.; Schuster, O.; Menke, G.

7.
РЖ ВИНИТИ 76 (BI31) 95.10-04Т3.14

   

    Excretion of centchroman in breast milk [Text] / J. K. Paliwal [et al.] // Brit. J. Clin. Pharmacol. - 1994. - Vol. 38, N 5. - P485-486 . - ISSN 0306-5251
Перевод заглавия: Экскреция центхрома в грудное молоко
ГРНТИ  
ВИНИТИ 761.31.29.02.09
Рубрики: ФАРМАКОКИНЕТИКА
ЦЕНТХРОМ

ДОЗЫ

ФАРМАКОКИНЕТИЧЕСКИЕ ПАРАМЕТРЫ

СОДЕРЖАНИЕ В ГРУДНОМ МОЛОКЕ

СОДЕРЖАНИЕ В СЫВОРОТКЕ

ЗДОРОВЫЕ ИСПЫТУЕМЫЕ


Доп.точки доступа:
Paliwal, J.K.; Grover, P.K.; Asthana, O.P.; Nityanand, S.; Gupta, R.C.

8.
РЖ ВИНИТИ 76 (BI31) 95.10-04Т3.15

   

    Изучение фармакокинетики и биоэквивалентности ацетаминофена при пероральном применении капель у здоровых испытуемых [Text] / Zheng Hong [et al.] // Huaxi yike daxue xuebao = J. West China Univ. Med. Sci. - 1994. - Vol. 25, N 4. - С. 410-413 . - ISSN 0257-7712
Аннотация: The concentrations of acetaminophen in human plasma were determined by RP-HPLC after administration of a single oral dose of 1000 mg acetaminophen oral drop or tablet to eight normal male volunteers a crossover study. The concentration vs time curves of acetaminophen all fitted the two compartment model. The C[max] in oral drop and tablet were 11.23'+-'0.93 and 8.79'+-'0.93 mg/L, respectively; T[max] were 0.86'+-'0.08 and 1.48'+-'0.39h; T[1/2'бета']3.03'+-'0.79 and 2.51'+-'1.10 h; AUC 42.35'+-'6.20 and 40.60'+-'6.79 mg/L* h. When AUC in tablet was 100%, the relative bioavailability of acetaminophen oral drop was 105.58%. The results showed that the oral drop and tablet are bioequivalent
ГРНТИ  
ВИНИТИ 761.31.29.02.09
Рубрики: ФАРМАКОКИНЕТИКА
АЦЕТАМИНОФЕН

КАПЛИ

ТАБЛЕТКИ

ПРИЕМ ВНУТРЬ

ФАРМАКОКИНЕТИЧЕСКИЕ ПАРАМЕТРЫ

БИОЭКВИВАЛЕНТНОСТЬ

СРАВНИТЕЛЬНЫЙ АНАЛИЗ

ЗДОРОВЫЕ ИСПЫТУЕМЫЕ


Доп.точки доступа:
Hong, Zheng; Li, Zhangwan; Wang, Yusheng; Li, Lianghong; Qiang, Wenan; Wang, Mu; Zou, Jigen

9.
РЖ ВИНИТИ 76 (BI31) 95.10-04Т3.18

   

    Do steroids influence low dose methotrexate pharmacokinetics? [Text] : comment / P. Lafforgue [et al.] // J. Rheumatol. - 1994. - Vol. 21, N 6. - P1170-1171 . - ISSN 0315-162X
Перевод заглавия: Влияют ли стероиды на фармакокинетику метотрексата в низких дозах?
ГРНТИ  
ВИНИТИ 761.31.29.02.17
Рубрики: РЕВМАТИЧЕСКИЕ ЗАБОЛЕВАНИЯ
КОРТИКОСТЕРОИДЫ

ДОЗЫ

МЕТОТРЕКСАТ

НИЗКИЕ ДОЗЫ

ФАРМАКОКИНЕТИЧЕСКИЕ ПАРАМЕТРЫ

БОЛЬНЫЕ


Доп.точки доступа:
Lafforgue, P.; Monjanel-Mouterde, S.; Durand, A.; Catalin, J.; Acquaviva, P.G.

10.
РЖ ВИНИТИ 76 (BI31) 95.10-04Т3.212

    Kremer, Joel M.

    Examination of pharmacokinetic variables in a cohort of patients with rheumatoid arthritis beginning therapy with methotrexate compared with a cohort receiving the drug for a mean of 81 months [Text] / Joel M. Kremer, Gayle F. Petrillo, Robert A. Hamilton // J. Rheumatol. - 1995. - Vol. 22, N 1. - P41-44 . - ISSN 0315-162X
Перевод заглавия: Исследование фармакокинетических различий у больных ревматоидным артритом в начале лечения метотрексатом в сравнении с больными, получавшими его в качестве основного лекарственного средства в течение 81 месяца
Аннотация: To compare pharmacokinetic variables of a 7.5 mg dose of MTX in a cohort of patients with rheumatoid arthritis (RA) beginning therapy with the drug with a cohort of patients receiving the drug for a mean period of 81 months. Methods. Standard pharmacokinetic measures were performend in 35 patients beginning MTX therapy and 15 patients who had received the drug for a mean of 81 months. Results. No significant differences in area under the serum concentration versus time curve (AUC), maximal methotrexate concentration following dosing (C[max]), time to C[max] (T[max]), bioavailability (F), urinary MTX, renal clearance of MTX or creatinine clearance were observed between the 2 cohorts. Conclusion. We were unable to demonstrate significant differences in pharmacokinetic variables in these cohorts with a 7.5 mg standard dose of MTX. It is possible that a difference may exist when a standard higher dose of MTX is compared in these types of patients
ГРНТИ  
ВИНИТИ 761.31.29.23.11.09
Рубрики: РЕВМАТОИДНЫЙ АРТРИТ
МЕТОТРЕКСАТ

ДОЗА

ФАРМАКОКИНЕТИЧЕСКИЕ ПАРАМЕТРЫ

НАЧАЛЬНАЯ ТЕРАПИЯ

ДЛИТЕЛЬНАЯ ТЕРАПИЯ

СРАВНИТЕЛЬНЫЙ АНАЛИЗ

БОЛЬНЫЕ


Доп.точки доступа:
Petrillo, Gayle F.; Hamilton, Robert A.

11.
РЖ ВИНИТИ 76 (BI31) 95.11-04Т3.15

   

    Repeated dose pharmacokinetics of pancopride in human volunteers [Text] / P. Salva [et al.] // Biopharm. and Drug Dispos. - 1994. - Vol. 15, N 8. - P643-651 . - ISSN 0142-2782
Перевод заглавия: Фармакокинетика повторной дозы панкоприда у здоровых испытуемых
Аннотация: The aim of this study was to assess the pharmacokinetic profile of pancopride after repeated oral dose administration of 20 mg pancopride in tablet form once a day for 5 d in 12 healthy male volunteers. Plasma levels were measured by HPLC using a solid phase extraction method and automated injection. The minimum quantification limit of pancopride in plasma was 2 ng mL{-1}. The maximum plasma concentration (mean'+-'SD) after the first dose was 92*5'+-'41*5 ng mL{-1} and t[max] was 1*7'+-'0*9 h. The elimination half-life (t[1/2]) was 14*3'+-'6*9 h. The area under the concentration-time curve from zero to infinity (AUC) was 997'+-'396 ng h mL{-1}. The maximum plasma concentration (mean'+-'SD) at steady state (day 5) was 101*8'+-'36*9 ng mL{-1} and t[max] was 2*2'+-'1*2 h. The elimination half-life (t[1/2]) was 16*3'+-'2*7 h and the minimum plasma concentration (C{ss}[min]) was 16*6'+-'6*9 ng mL{-1}. The area under the concentration-time curve during the dosing interval (AUC{ss}[r]) was 995'+-'389 ng h mL{-1}. The average plasma concentration at steady state (C{ss}[av]) was 43*3'+-'16*1 ng mL{-1} and the expetimental accumulation ratio (R[AUC]) was 1*34'+-'0*19, whereas the mean theoretical value (R) was 1*40'+-'0*29. The results obtained showed a good correlation between the experimental plasma levels and the expected values calculated using a repeated dose two-compartment model assessed by means of the Akaike value. It is concluded that the pharmacokinetics of pancopride are not modified after repeated dose administration. The safety parameters showed no clinically relevant alterations
ГРНТИ  
ВИНИТИ 761.31.29.02.09
Рубрики: ПАНКОПРИД
ДОЗЫ

ПОВТОРНОСТЬ ДОЗ

ПРОДОЛЖИТЕЛЬНОСТЬ ПРИМЕНЕНИЯ

ФАРМАКОКИНЕТИЧЕСКИЕ ПАРАМЕТРЫ

ЗДОРОВЫЕ ИСПЫТУЕМЫЕ


Доп.точки доступа:
Salva, P.; Costa, J.; Perez-Campos, A.; Martinez-Tobed, A.

12.
РЖ ВИНИТИ 76 (BI31) 95.11-04Т3.16

   

    Pharmacokinetics and biochemical efficacy of idrapril calcium, a novel ACE inhibitor, after multiple oral administration in humans [Text] / P. J. Wyld [et al.] // Brit. J. Clin. Pharmacol. - 1994. - Vol. 38, N 5. - P421-425 . - ISSN 0306-5251
Перевод заглавия: Фармакокинетика и биохимическая активность идраприла кальция, нового ингибитора ангиотензин-конвертирующего фермента, после многократного приема внутрь у людей
Аннотация: The pharmacokinetic profile and biochemical efficacy of idrapril calcium, a novel angiotensin converting enzyme (ACE) inhibitor, were evaluated in bealthy volunteers after multiple dosing for 5 days at the doses of 100, 200 and 400 mg twice daily. The study was conducted as a double-blind, cross-over comparison of idrapril calcium against placebo. Plasma concentrations of idrapril were determined by an indirect enzymatic method. Urinary concentrations were measured by reverse phase high performance liquid chromatography (h.p.l.c.). Plasma samples were also analysed for ACE activity. The pharmacokinetics of idrapril calcium did not change cignificantly between day 1 and day 5. The values of C[max] and AUC were dose-related over the range of doses tested; t[max] was 3-4 h and apparent elimination half-life was 1.4-1.6 h. Plasma ACE activity was maximally inhibited (94-96%) at all dose levels and remained more than 80% depressed from 2 to at least 6 h after idrapril calcium. Although the maximum effect was not dose-related, the duration of inhibition showed some dose-dependency. ACE activity returning to 56, 45 and 29% of the basal value 12 h after the 100, 200 and 400 mg doses, respectively. There were no clinically significant adverse events experienced by the volunteers. No dose-telated effects on blood pressure or heart rate were observed. There were no changes in clinical pathology tests, urine analyses or electrocardiograms after dosing with idrapril calcium. Idrapril calcium, the prototype of a new class of ACE inhibitors, appears to be well-tolerated. Its pharmacokinetics were not significantly changed after repeated administration in man. Plasma ACE activity was markedly depressed for more than 12 h even after the lowest dose tested (100 mg) and inhibition was correlated to the levels of circulating drug, the ex vivo IC[50] being practically identical (12 ng ml{-1}) on day 1 and day 5
ГРНТИ  
ВИНИТИ 761.31.29.02.09
Рубрики: ФАРМАКОКИНЕТИКА
ИДРАПРИЛА КАЛЬЦИЙ

ДОЗЫ

ПРИЕМ ВНУТРЬ

ФАРМАКОКИНЕТИЧЕСКИЕ ПАРАМЕТРЫ

ПОБОЧНЫЕ ЭФФЕКТЫ

ЗДОРОВЫЕ ИСПЫТУЕМЫЕ


Доп.точки доступа:
Wyld, P.J.; Grant, J.; Lippi, A.; Criscuoli, M.; Del, Re G.; Subissi, A.

13.
РЖ ВИНИТИ 76 (BI31) 95.11-04Т3.18

    Nahata, Milap C.

    Pharmacokinetics of cefpirome in pediatric patients [Text] : [Abstr.] Annu. Meet. Amer. Coll. Clin. Pharm., St. Louis, Mo, July 31-Aug.3, 1994 / Milap C. Nahata, William J. Barson, Surendra K. Puri // Pharmacotherapy. - 1994. - Vol. 14, N 3. - P369-370 . - ISSN 0277-0008
Перевод заглавия: Фармакокинетика цефпирома у больных детей
Аннотация: Cefpirome is an investigational antibiotic with antimicrobial astibity comparable to third-generation cephalosporins. We designed a study to determine the pharmacokinetics and tolerance of cefpirome in pediatric patients. A single dose of cefpirome was administered IV over 15 minutes to 13 patients (age 0.5-13 years). The dose was 10 m g/kg in four patients, 25 mg/kg in five, and 50 mg/kg in four patients. Blood samples were collected at 0, 0.25, 0.5, 1, 3, 5, and 8 hours after the dose, and cefpirome was measures by an HPLC method. The maximium serum soncentration ranged from about 53.6 to 454 'мю'g/ml. The mean total body clearance, appatent volume of distribution, and elimination half-life was 2.15'+-'0.70 ml/min/kg, 0.32'+-'0.32 l/kg, and 1.8'+-'1.3 hr, respectively Pharmacokinetics was independent of dose. No significant adverse effects were attributed to celpirome. These data may be useful in conducting efficacy and safety studies of celpirome in pediatric patients
ГРНТИ  
ВИНИТИ 761.31.29.02.09
Рубрики: ФАРМАКОКИНЕТИКА
ЦЕФПИРОМ

ДОЗЫ

ФАРМАКОКИНЕТИЧЕСКИЕ ПАРАМЕТРЫ

БОЛЬНЫЕ ДЕТИ


Доп.точки доступа:
Barson, William J.; Puri, Surendra K.

14.
РЖ ВИНИТИ 76 (BI31) 95.11-04Т3.109

    Jensen, Moller K.

    Plasma concentrations of glyceryl trinitrate and its dinitrate metabolites after sublingual administration to volunteers [Text] / Moller K. Jensen, Berg J. Dahl // Arzneim.-Forsch. - 1994. - Vol. 44, N 8. - P951-953 . - ISSN 0004-4172
Перевод заглавия: Содержание глицерина тринитрата и его динитратных метаболитов в крови после сублингвального применения
Аннотация: The plasma profiles of nitroglycerin (glyceryl trinitrate, GTN, CAS 55-63-0) and its dinitrate metabolites (1,2-GDN and 1,3-GDN) were estimated after sublingual administration of GTN tablets 0.5 mg (Nitromex{R}) given in single doses to 20 volunteers. Blood samples (totally 20) were collected to 2 h after administration, and the plasma concentrations of GTN, 1,2-GDN, and 1,3-GDN were measured simultaneously by gas chromatography: The pharmacokinetic parameters, C[max], t[max], t[1/2], and the dinitrate ratio (AUC[1,2-GDN]/AUC[1,3-GDN]) were determined for each subject. The plasma concentrations of GTN reached a maximum of 1.38 ng/ml (mean) (range: 0.32-3.18 ng/ml) after 4.9 min (mean) (range: 3-8 min). The plasma concentrations of 1,2-GDN and 1,3-GDN reached a maximum of 3.11 ng/ml (mean) (range: 1.14-5.44 ng/ml) and 0.70 ng/ml (mean) (range: 0.33-1.19 ng/ml) after 13.7 min (mean) (range: 8-40 min) and 17.6 min (mean) (range: 8-40 min). The t[1/2] values (mean) were 3.3, 35.5, and 38.1 min for GTN, 1,2-GDN, and 1,3-GDN, respectively. The dinitrate ratio was estimated to be 4.1 (mean)
ГРНТИ  
ВИНИТИ 761.31.29.11.09.07
Рубрики: ГЛИЦЕРИНА ТРИНИТРАТ
ГЛИЦЕРИНА ТРИНИТРАТ*1,2-

ГЛИЦЕРИНА ТРИНИТРАТ*1,3-

ТАБЛЕТКИ

ДОЗЫ

СУБЛИНГВАЛЬНОЕ ПРИМЕНЕНИЕ

ФАРМАКОКИНЕТИЧЕСКИЕ ПАРАМЕТРЫ

ЗДОРОВЫЕ ИСПЫТУЕМЫЕ


Доп.точки доступа:
Dahl, Berg J.

15.
РЖ ВИНИТИ 76 (BI40) 95.12-04М7.408

    Kremer, Joel M.

    Examination of pharmacokinetic variables in a cohort of patients with rheumatoid arthritis beginning therapy with methotrexate compared with a cohort receiving the drug for a mean of 81 months [Text] / Joel M. Kremer, Gayle F. Petrillo, Robert A. Hamilton // J. Rheumatol. - 1995. - Vol. 22, N 1. - P41-44 . - ISSN 0315-162X
Перевод заглавия: Исследование фармакокинетических различий у больных ревматоидным артритом в начале лечения метотрексатом в сравнении с больными, получавшими его в качестве основного лекарственного средства в течение 81 месяца
Аннотация: To compare pharmacokinetic variables of a 7.5 mg dose of MTX in a cohort of patients with rheumatoid arthritis (RA) beginning therapy with the drug with a cohort of patients receiving the drug for a mean period of 81 months. Methods. Standard pharmacokinetic measures were performend in 35 patients beginning MTX therapy and 15 patients who had received the drug for a mean of 81 months. Results. No significant differences in area under the serum concentration versus time curve (AUC), maximal methotrexate concentration following dosing (C[max]), time to C[max] (T[max]), bioavailability (F), urinary MTX, renal clearance of MTX or creatinine clearance were observed between the 2 cohorts. Conclusion. We were unable to demonstrate significant differences in pharmacokinetic variables in these cohorts with a 7.5 mg standard dose of MTX. It is possible that a difference may exist when a standard higher dose of MTX is compared in these types of patients
ГРНТИ  
ВИНИТИ 761.03.49.51.31.25
Рубрики: РЕВМАТОИДНЫЙ АРТРИТ
МЕТОТРЕКСАТ

ДОЗА

ФАРМАКОКИНЕТИЧЕСКИЕ ПАРАМЕТРЫ

НАЧАЛЬНАЯ ТЕРАПИЯ

ДЛИТЕЛЬНАЯ ТЕРАПИЯ

СРАВНИТЕЛЬНЫЙ АНАЛИЗ

БОЛЬНЫЕ


Доп.точки доступа:
Petrillo, Gayle F.; Hamilton, Robert A.

16.
РЖ ВИНИТИ 34 (BI48) 96.02-04Т2.474

   

    Prediction of brain delivery of ofloxacin, a new quinolone, in the human from animal data [Text] / Junichi Kawakami [et al.] // J. Pharmacokinet. and Biopharm. - 1994. - Vol. 22, N 3. - P207-227 . - ISSN 0090-466X
Перевод заглавия: [Изучение возможности] доставки нового хинолона офлоксацина в мозг человека на основании результатов, полученных в экспериментах на животных
Аннотация: На основании физиологических св-в и фармакокинетических параметров различных антибактериальных средств у разных видов животных провели оценку доставки офлоксацина (I) в спинномозговую жидкость (СМЖ) человека. Методами корреляционного анализа вычислили величины клиренса при диффузии I из крови в СМЖ, кажущегося объема распределения и общего клиренса I. Все параметры, вычисленные по экспериментальным данным у животных, хорошо согласовывались с клиническими результатами. Япония, Faculty of Medicine, The Univ. of Tokyo, Tokyo 113. Библ. 75
ГРНТИ  
ВИНИТИ 341.45.21.95.17.11
Рубрики: ОФЛОКСАЦИН
ДОСТАВКА В МОЗГ

СПИННОМОЗГОВАЯ ЖИДКОСТЬ

КОНЦЕНТРАЦИИ

ФАРМАКОКИНЕТИЧЕСКИЕ ПАРАМЕТРЫ

ЧЕЛОВЕК

ЭКСПЕРИМЕНТАЛЬНЫЕ ЖИВОТНЫЕ

ЭКСТРАПОЛЯЦИЯ ДАННЫХ


Доп.точки доступа:
Kawakami, Junichi; Yamamoto, Koujirou; Sawada, Yasufumi; Iga, Tatsuji

17.
РЖ ВИНИТИ 34 (BI48) 96.05-04Т1.24

    Ritter, James M.

    PET: A symposium highlighting its clinical and pharmacological potential [Text] / James M. Ritter, Terry Jones // Trends Pharmacol. Sci. - 1995. - Vol. 16, N 4. - P117-119 . - ISSN 0165-6147
Перевод заглавия: Позитронно-эмиссионная томография: симпозиум, освещающий ее клинические и фармакологические возможности
Аннотация: Обсуждены возможности позитронно-эмиссионной томографии (ПЭТ) для оценки фармакокинетических параметров соединений, меченных {15}O, {18}F и {11}C. Приведены примеры применения ПЭТ для изучения состояния мозгового кровообращения и метаболизма в мозге глюкозы, для характеристики нервных аппаратов миокарда, для скрининга противоопухолевых препаратов и др. Обращено внимание на роль ПЭТ в разработке новых лекарственных средств. Великобритания, Guy's Hospital, London SE1 9RT
ГРНТИ  
ВИНИТИ 341.45.01.13 + 341.45.05.05
Рубрики: МЕТОДЫ ИССЛЕДОВАНИЯ
ПОЗИТРОННО-ЭМИССИОННАЯ ТОМОГРАФИЯ

СИМПОЗИУМ

ФАРМАКОКИНЕТИЧЕСКИЕ ПАРАМЕТРЫ

ЛЕКАРСТВЕННЫЕ СРЕДСТВА


Доп.точки доступа:
Jones, Terry

18.
РЖ ВИНИТИ 34 (BI36) 96.08-04А4.361

    Ritter, James M.

    PET: A symposium highlighting its clinical and pharmacological potential [Text] / James M. Ritter, Terry Jones // Trends Pharmacol. Sci. - 1995. - Vol. 16, N 4. - P117-119 . - ISSN 0165-6147
Перевод заглавия: Позитронно-эмиссионная томография: симпозиум, освещающий ее клинические и фармакологические возможности
Аннотация: Обсуждены возможности позитронно-эмиссионной томографии (ПЭТ) для оценки фармакокинетических параметров соединений, меченных {15}O, {18}F и {11}C. Приведены примеры применения ПЭТ для изучения состояния мозгового кровообращения и метаболизма в мозге глюкозы, для характеристики нервных аппаратов миокарда, для скрининга противоопухолевых препаратов и др. Обращено внимание на роль ПЭТ в разработке новых лекарственных средств. Великобритания, Guy's Hospital, London SE1 9RT
ГРНТИ  
ВИНИТИ 341.49.33.15.15
Рубрики: МЕТОДЫ ИССЛЕДОВАНИЯ
ПОЗИТРОННО-ЭМИССИОННАЯ ТОМОГРАФИЯ

СИМПОЗИУМ

ФАРМАКОКИНЕТИЧЕСКИЕ ПАРАМЕТРЫ

ЛЕКАРСТВЕННЫЕ СРЕДСТВА


Доп.точки доступа:
Jones, Terry

19.
РЖ ВИНИТИ 34 (BI48) 96.11-04Т1.110

    Ma, Quanhua.

    Мониторинг концентрации аминофиллина в крови и расчет параметров фармакокинетики методом трех точек [Text] / Quanhua Ma, Xuzhuo Liu, Meiling Wang // Zhongguo yaoxue zazhi = Chin. Pharm. J. - 1995. - Vol. 30, N 8. - С. 482-484 . - ISSN 1001-2494
Аннотация: Методом трех точек рассчитаны значения K, T[1/2], V[d] и Cl, к-рые для аминофиллина составили 0,101 ч{-1}, 7,56 ч, 0,477 л*кг{-1} и 0,046 л*кг{-1}*ч{-1} соотв. Обсуждены преимущества метода. КНР, Shandong, Yidu Med. Sch., Qingzhou 262500. Библ. 2
ГРНТИ  
ВИНИТИ 341.45.15.09.05
Рубрики: ЭУФИЛЛИН
КОНЦЕНТРАЦИЯ В КРОВИ

ФАРМАКОКИНЕТИЧЕСКИЕ ПАРАМЕТРЫ

МЕТОД "ТРЕХ ТОЧЕК"


Доп.точки доступа:
Liu, Xuzhuo; Wang, Meiling

20.
РЖ ВИНИТИ 34 (BI48) 96.11-04Т1.116

    Chow, Shein-Chung.

    Assessment of bioequivalence using a multiplicative model [Text] / Shein-Chung Chow, Karl E. Peace, Jun Shao // J. Biopharm. Statist. - 1991. - Vol. 1, N 2. - P193-203 . - ISSN 1054-3406
Перевод заглавия: Оценка биоэквивалентности с использованием мультипликативной модели
Аннотация: Разработана система логарифмической трансформации фармакокинетических параметров (AUC, C[макс.] и t[макс.]) в целях оптимизации характеристики биоэквивалентности. США, Bristol-Myers Squibb Company, Plainsboro, NJ 08536. Библ. 10
ГРНТИ  
ВИНИТИ 341.45.15.09.05
Рубрики: БИОЭКВИВАЛЕНТНОСТЬ
ОПТИМИЗАЦИЯ ХАРАКТЕРИСТИКИ

ФАРМАКОКИНЕТИЧЕСКИЕ ПАРАМЕТРЫ

МУЛЬТИПЛИКАТИВНАЯ МОДЕЛЬ


Доп.точки доступа:
Peace, Karl E.; Shao, Jun

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